1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. GABA Receptor
    Cytochrome P450
  3. Clomethiazole

Clomethiazole 

Cat. No.: HY-129105 Purity: 98.19%
Handling Instructions

Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.

For research use only. We do not sell to patients.

Clomethiazole Chemical Structure

Clomethiazole Chemical Structure

CAS No. : 533-45-9

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Liquid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
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100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Chlormethiazole is an potent and orally active GABAA agonist[1]. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus[2].

In Vitro

Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1].
Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells, with EC50 values of 0.3 and 1.5 mM, respectively[1].
Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current[1].
Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 with IC50 values of 24 µM and 42 µM, respectively, in human liver microsomes, meanwhile all other isoforms exhibiting values > 300 µM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

161.65

Formula

C₆H₈ClNS

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1546.55 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.1862 mL 30.9310 mL 61.8621 mL
5 mM 1.2372 mL 6.1862 mL 12.3724 mL
10 mM 0.6186 mL 3.0931 mL 6.1862 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (12.87 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (12.87 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (12.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
Clomethiazole
Cat. No.:
HY-129105
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